antiviral drugs 2
Terms
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- acyclovir
-
nucleoside analog
converted to NuMP by viral thymidine kinase (infected cells only)
NuTP is a chain terminator
valacyclovir is prodrug that is better absorbed orally and can be given 3/day instead of 5/day
USES:
genital herpes (HSV)
herpes simples (HSV)
DRUG OF CHOICE FOR GENITAL HERPES (and herpes zoster, they're the same drugs): valaciclovir, acyclovir, and famiciclovir
DRUG OF CHOICE FOR NEONATAL HERPES: acyclovir (IV)
acyclovir is DRUG OF CHOICE FOR HERPES ENCEPHALITIS (even though vidarabine is the only one not approved) - what are the T4+ cell levels to begin treatment of HIV patient
-
symptomatic - treat
>350 dont treat
<200 treat
200-350 = grey area - interferon alpha-2a
-
viral transcription inhibitor
USES:
Hepatitis B
Hepatitis C (IFN alpha2 + ribavirin) - this is the only Rx recommended
s/e:
depression and flu-like syndrome
"feel like shit and depressed" - peginterferon alpha-2b
-
viral transcription inhibitor
polyethylene glycol increases its half life
inhibits viral transcription
USES:
Hepatitis B
Hepatitis C (IFN alpha2 + ribavirin)
s/e:
depression and flu-like syndrome - saquinavir
- protease inhibitor
- zalcitabine
- zal is a NRTI to be taken off the market because it is not very potent and sucks really bad
- atazanavir + indinavir?
- Artificial intelligence = hyperbilirubinemia
- amantandine
-
uncoating inhibitor (man in a coat)
inhbits viral uncoating
works only on Influenza type A (M2 ion channel) - rimantadine
-
uncoating inhibitor (man in a coat)
inhbits viral uncoating
works only on Influenza type A (M2 ion channel)
amantadine and rimantadine - very similar - fomivirsen
-
intraocular antiviral for CMV
antisense (german) oligo that inhibits translation
USES:
CMV retinitis (AIDS patients) - vidarabine
-
nucleoside analog
topically: herpes keratitis or conjunctivitis
DRUG OF CHOICE FOR HERPES KERATITIS: vidarabine, idoxurine, trifluridine
IV: herpes encephalitis (acyclovir works better) - penciclovir
-
nucleoside analog
activated by thymidine kinased (like acyclovir) so selective
cream: oral herpes simplex (cold sores)
DRUG OF CHOICE FOR ORAL HERPES: pen and fam - famiclovir
-
nucleoside analog. prodrug of penciclovir.
activated by thymidine kinase so it's selective.
Use: herpes simplex (I'm not a fam of cold sores)
DRUG OF CHOICE FOR ORAL HERPES: pen and fam
DRUG OF CHOICE FOR GENITAL HERPES (and herpes zoster, they're the same drugs): valaciclovir, acyclovir, and famiciclovir - trifluridine
-
ophthalmic antiviral for HSV keratitis
DRUG OF CHOICE FOR HERPES KERATITIS: vidarabine, idoxurine, trifluridine - idoxurine
-
ophthalmic antiviral for HSV keratitis
DRUG OF CHOICE FOR HERPES KERATITIS: vidarabine, idoxurine, trifluridine - ganciclovir
-
inhibits CMV polymerase (comp inhib for active site)
converted to Ganciclovir-MP by UL97 (CMV enzyme)
S/E:
bone marrow suppression
prodrug: valciclovir (can give orally instead of IV)
drugs for CMV: ganciclovir, valganciclovir, foscarnet, cidofovir, fomivirsen - foscarnet
-
pyrophosphate analog
*doesnt have to be phosphorylated to be activated*
competitively inhibits herpesvirus family DNA pol
USE: CMV retinitis
***s/E (3):
1. nephrotoxic (think renal transplant patients)
2. electrolyte disturbances
3. seizures
drugs for CMV: ganciclovir, valganciclovir, foscarnet, cidofovir, fomivirsen - cidofovir
-
nucleoside analog
**converted by cellular enzymes to a Nucleotide DI-Phoshate!
chain terminator
**administered with probenecid which blocks its secretion
s/e: nephrotoxicity - (think renal transplant patients)
USE: CMV, CMV retinitis (use with ganciclovir)
drugs for CMV: ganciclovir, valganciclovir, foscarnet, cidofovir, fomivirsen - ribavirin
-
monophosphate dehydrogease inhibitor, blocking synthesis of dGTP. inhibits RNA polymerase of influenza virus
USES:
Influenza
RSV
chronic Hepatitis C virus (ribavirin + pegIFN 2 alpha b)
this is the only Rx recommended - LAMIVUDINE
-
* NRTI - works on HIV and HBV
nucleoside analog. chain terminator
HIV & HBV drug. emtricitabine and lamivudine are similar. DONT USE TOGETHER
USES:
HIV
hepatitis B
low cytotoxicity (few side effects)
Hep B = ALEE
adefovir
lamivudine
entacavir
emtricetabine - emtricitabine
-
* NRTI - works on HIV and HBV
nucleoside analog. chain terminator
HIV & HBV drug. emtricitabine and lamivudine are similar. DONT USE TOGETHER!
USES:
HIV
hepatitis B - adevofir dipivol
-
chain terminator
USE: hepatitis B - entacavir
-
nucleoside analog
USE: hepatitis B
Hep B = ALEE
adevofir
LAMIVUDINE
entacavir
emtricetabine - zanamivir
-
neuraminidase inhibitor
USE:
Influenza type A and B
give prophylactically to family member or <2 days after symptoms - oseltamivir
-
neuraminidase inhibitor
USE:
Influenza type A and B
give prophylactically to family member or <2 days after symptoms - enfuvirtide
-
enFUvirtide is a FUSION INHIBITOR antiretroviral
it binds the gp41 (tm) and prevents conf changes - tenofovir
- NRTI - new drug and very potent
- zidovudine
-
* NRTI
DONT GIVE WITH stavudine!
a pregnancy monotherapy - didanosine
-
* NRTI
s/e: peripheral neuropathy - efavirenz
-
* nNRTI (only 2 of these)
efavirenz (fuck the virenz!)
teratogenic. do not give during pregnancy. use nevirapine instead (the other nNRTI)
s/e: hallucination dreams
rash / stevens johnsons! - nevirapine
-
* nNRTI
nevirapine (never a nucleotide) = nN
mostly to prevent mother -> child HIV transmission (monotherapy.)
never transmit HIV to a child. - lopinavir
-
lopinavir / r
protease inhibitor
dual PI therapy = ritonavir is given in a low dose mainly to inhibit CYP450 and increase levels of other protease inhibitors - ritonavir
-
protease inhibitor
can be given in a low dose to inhibit CYP450 and increase levels of other protease inhibitors - side fx of protease inhibitors
-
buffalo hump
peripheral lipodystrophy
elevated triglycerides, elevated total cholesterol
hyperglycemia / insulin resistance - stavudine
-
NTRI
known for peripheral neuropathy
DONT GIVE WITH zidovudine! - HAART NNTRI therapy
-
2 NTRI + NNTRI
NNTRI's: efavirenz and nevirapine
never eff dudes and you wont need these - HAART PI therapy
- 2 NTRI + PI